Related Experiment Video
Updated: May 25, 2026

An In-House-Built and Light-Emitting-Diode-Based Photodynamic Therapy Device for Enhancing Verteporfin Cytotoxicity in a 2D Cell Culture Model
Published on: January 13, 2023
Drug targeting strategies for photodynamic therapy
Frédéric Schmitt1, Lucienne Juillerat-Jeanneret
1Institute of Pathology, University Hospital of Lausanne, CHUV-UNIL Bugnon 25, CH-1011 Lausanne, Switzerland.
Abstract:
In human pathologies, therapeutic treatments are often limited by the lack of selectivity of drugs and their elevated effective concentrations. Targeting these agents to a defined tissue could enhance their selectivity and then diminish their side effects when compared to drugs that accumulate in the entire body. Targeting could also improve treatment efficiency by allowing a localized high concentration of the agents. Based on the different behaviors and patterns of expression between diseased and normal cells, strategies for targeting can be explored. For example, receptors, proteases or trans-membrane carriers could be different or differently expressed. Many therapeutic procedures rely on this fact, including photodynamic therapy (PDT). PDT is already used in the treatment of some cancers, of inflammatory diseases and others diseases such as age-related macular degeneration or acne. PDT relies on the activation of a photosensitizer (PS) by visible light which results in the production of cytotoxic reactive oxygen species. In PDT, the general distribution of PS to the whole body leads to generalized photosensitization and poor acceptance of treatments by patients. One way to avoid these effects is to improve the targeting of PSs to diseased tissues using modification of PS with peptides or proteins that will target specific receptors or enzymes. PSs could also be functionalized with non-proteic ligands such as organometalics to achieve targeted and/or combined therapies. Alternatively, PSs could be encapsulated in nanoparticles bearing targeting agents which will decrease concentration of free circulating PS and improve photodynamic efficiency. These different approaches will be discussed in the present review with an emphasis on the use of peptides and proteins.
Insights
Targeting drugs to specific tissues enhances selectivity and reduces side effects. This review explores methods like peptide and protein modifications for targeted photodynamic therapy (PDT) to improve treatment efficacy.
Area of Science:
- Biomedical Engineering
- Drug Delivery Systems
- Photodynamic Therapy
Background:
- Therapeutic treatments face limitations due to drug non-selectivity and high effective concentrations, leading to side effects.
- Targeting drugs to specific tissues can improve selectivity, reduce systemic toxicity, and enhance therapeutic efficiency.
- Photodynamic therapy (PDT) utilizes photosensitizers (PS) activated by light to produce cytotoxic species, but systemic PS distribution causes generalized photosensitization.
Purpose of the Study:
- To review strategies for improving the targeting of photosensitizers (PSs) in photodynamic therapy (PDT).
- To discuss methods for enhancing PS selectivity towards diseased tissues, thereby minimizing side effects.
- To emphasize the role of peptides and proteins in targeted PDT approaches.
Main Methods:
- Review of existing literature on drug targeting strategies in human pathologies.
- Analysis of methods to modify photosensitizers (PSs) for enhanced tissue-specific accumulation.
- Exploration of targeting agents including peptides, proteins, non-proteic ligands, and nanoparticles.
Main Results:
- Targeting strategies can exploit differences in receptor expression or enzyme activity between diseased and normal cells.
- Modification of PSs with peptides, proteins, or encapsulation in nanoparticles can improve targeting efficiency.
- Functionalization with organometallic ligands offers potential for targeted and combined therapies.
Conclusions:
- Targeted delivery of photosensitizers (PSs) is crucial for improving the efficacy and patient acceptance of photodynamic therapy (PDT).
- Peptide and protein-mediated targeting, along with nanoparticle encapsulation, represent promising avenues for advanced PDT.
- Further research into targeted therapies can overcome current limitations in treating various human pathologies.
Related Concept Videos
Modified-Release Drug Delivery Systems: Site-Targeted
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

